Design, synthesis and biological evaluation of thieno[3,2-c]pyrazol-urea derivatives as potent glycogen synthase kinase 3β inhibitors based on the DFG-out conformation.

Glycogen synthase kinase 3β (GSK-3β) is a potential therapeutic target for the treatment of a variety of human diseases. Here, we report the design and synthesis of a series of thieno[3,2-c]pyrazol-urea derivatives and evaluation of their GSK-3β inhibitory activity. Among these analogues, the compound without substitution on terminal phenyl ring (3a) was found to be the most potent GSK-3β inhibitor with an IC of 74.

SIRT1-dependent deacetylation of Txnip H3K9ac is critical for exenatide-improved diabetic kidney disease.

Glucagon-like peptide 1 receptor agonist exenatide (exendin-4) has potential protective capabilities against diabetic kidney disease (DKD). However, the underlying mechanism has not been fully elucidated. The expression of thioredoxin-interacting protein (Txnip) is upregulated during DKD progression by histone acetylation.

Lifestyle and Social Factors Exacerbated on the Prevalence of Mood Disorders and Functional Dyspepsia Among Neonatal Nurses in China.

Background: Nursing is a high-stress occupation that can have an impact on mental health, particularly for neonatal nurses. Job-related stress factors and work-related behaviors have played a critical role in nurses' mental health. This study aimed to explore the prevalence of mood disorders and the impact of social factors, lifestyle on mood disorders among neonatal nurses.

GR-1 Ameliorates -Induced Activation of NLRP3 and NLRC4 Inflammasomes With Differential Requirement for ASC.

is a common cause of mastitis in dairy cows. The adaptor protein apoptosis-associated speck-like protein containing a caspase recruitment domain (ASC) synergizes with caspase-1 to regulate inflammasome activation during pathogen infection. Here, the gene was knocked out in bovine mammary epithelial (MAC-T) cells using clustered, regularly interspaced, short palindromic repeat (CRISPR)/CRISPR-associated (Cas)-9 technology.